Catalog No.: PC-72049Not For Human Use, Lab Use Only.
M5049 (Enpatoran, M-5049) is a novel potent, selective TLR7/8 inhibitor with IC50 of 11.1/24.1 nM in HEK NF-kB-luciferase reporter cells assay, repectively
M5049 (Enpatoran, M-5049) is a novel potent, selective TLR7/8 inhibitor with IC50 of 11.1/24.1 nM in HEK NF-kB-luciferase reporter cells assay, repectively.
M5049 (Enpatoran) is potent against TLR7 and TLR8 in PBMCs (IL-6 IC50=68.3 and 620 nM) as well as whole blood (IL-6 IC50=2.2 nM).
M5049 (Enpatoran) showed good selectivity and were found to be inactive against TLR3,TLR4 and TLR9 in vitro and in vivo, as wll as against a panel of 389 kinases as off-target profiling and at 1 mM M5049 only inhibited the activity of one kinase more than 50% (CAMKK2)
M5049 (Enpatoran) blocks multiple TLR7/8 RNA ligands. Treatment of BXSB-Yaa mice with M5049 (Enpatoran) led to an improvement in survival and reduction in kidney disease as evidenced by lower proteinuria.
